Controlled release and taste masking oral pharmaceutical composition

Abstract

Controlled release and taste masking compositions containing one or more active principles inglobated in a three-component matrix structure, i.e. a structure formed by successive amphiphilic, lipophilic or inert matrices and finally inglobated or dispersed in hydrophilic matrices. The use of a plurality of systems for the control of the dissolution of the active ingredient modulates the dissolution rate of the active ingredient in aqueous and/or biological fluids, thereby controlling the release kinetics in the gastrointestinal tract.

1 . A controlled release oral pharmaceutical composition, comprising budesonide and wherein said composition provides an in vitro release rate of said budesonide at pH 7.2 such that less than 15% of said budesonide is released after 1 hour, 25% to 55% of said budesonide is released after 4 hours, and more than 80% of said budesonide is released after 8 hours. 
     
     
         2 . A controlled release oral pharmaceutical composition according to  claim 1 , wherein said composition releases less than 25% of said budesonide after 2 hours. 
     
     
         3 . A controlled release oral pharmaceutical composition according to  claim 1 , wherein said composition releases less than 5% of said budesonide after 2 hours at pH 1. 
     
     
         4 . A controlled release oral pharmaceutical composition according to  claim 2 , wherein said composition releases less than 5% of said budesonide after 2 hours at pH 1. 
     
     
         5 . A controlled release oral pharmaceutical composition according to  claim 1 , wherein said composition releases less than 5% of said budesonide after 1 hour at pH 6.4. 
     
     
         6 . A controlled release oral pharmaceutical composition according to  claim 2 , wherein said composition releases less than 5% of said budesonide after 1 hour at pH 6.4. 
     
     
         7 . A controlled release oral pharmaceutical composition according to  claim 3 , wherein said composition releases less than 5% of said budesonide after 1 hour at pH 6.4. 
     
     
         8 . A controlled release oral pharmaceutical composition according to  claim 4 , wherein said composition releases less than 5% of said budesonide after 1 hour at pH 6.4. 
     
     
         9 . A controlled release oral pharmaceutical composition according to  claim 1  comprising 9 mg of budesonide 
     
     
         10 . A controlled release oral pharmaceutical composition according to  claim 2  comprising 9 mg of budesonide. 
     
     
         11 . A controlled release oral pharmaceutical composition according to  claim 3  comprising 9 mg of budesonide. 
     
     
         12 . A controlled release oral pharmaceutical composition according to  claim 5  comprising 9 mg of budesonide. 
     
     
         13 . A method of treating a subject known to suffer from Inflammatory Bowel Disease or Irritable Bowel Syndrome comprising administering a therapeutically effective amount of the controlled release oral pharmaceutical composition according to  claim 1  to said subject in need of such treatment. 
     
     
         14 . A method of treating a subject known to suffer from Inflammatory Bowel Disease or Irritable Bowel Syndrome comprising administering a therapeutically effective amount of the controlled release oral pharmaceutical composition according to  claim 2  to said subject in need of such treatment. 
     
     
         15 . A method of treating a subject known to suffer from Inflammatory Bowel Disease or Irritable Bowel Syndrome comprising administering a therapeutically effective amount of the controlled release oral pharmaceutical composition according to  claim 3  to said subject in need of such treatment. 
     
     
         16 . A method of treating a subject known to suffer from Inflammatory Bowel Disease or Irritable Bowel Syndrome comprising administering a therapeutically effective amount of the controlled release oral pharmaceutical composition according to  claim 5  to said subject in need of such treatment. 
     
     
         17 . A method of treating a subject known to suffer from Inflammatory Bowel Disease or Irritable Bowel Syndrome comprising administering a therapeutically effective amount of the controlled release oral pharmaceutical composition according to  claim 9  to said subject in need of such treatment. 
     
     
         18 . A controlled release oral pharmaceutical composition, comprising budesonide and wherein said composition provides an in vitro release rate of said budesonide at pH 7.2 such that less than 10% to about 20% of said budesonide is released after 2 hours, 25% to 65% of said budesonide is released after 4 hours, and more than 80% of said budesonide is released after 8 hours. 
     
     
         19 . A controlled release oral pharmaceutical composition according to  claim 18 , wherein said composition releases less than 5% of said budesonide after 2 hours at pH 1. 
     
     
         20 . A controlled release oral pharmaceutical composition according to  claim 18 , wherein said composition releases less than about 5% of said budesonide after about 1 hour at pH 6.4. 
     
     
         21 . A controlled release oral pharmaceutical composition according to  claim 19 , wherein said composition releases less than about 5% of said budesonide after about 1 hour at pH 6.4. 
     
     
         22 . A controlled release oral pharmaceutical composition according to  claim 18  comprising 9 mg of budesonide. 
     
     
         23 . A controlled release oral pharmaceutical composition according to  claim 19  comprising 9 mg of budesonide. 
     
     
         24 . A controlled release oral pharmaceutical composition according to  claim 20  comprising 9 mg of budesonide. 
     
     
         25 . A controlled release oral pharmaceutical composition according to  claim 21  comprising 9 mg of budesonide. 
     
     
         26 . A method of treating a subject known to suffer from Inflammatory Bowel Disease or Irritable Bowel Syndrome comprising administering a therapeutically effective amount of the controlled release oral pharmaceutical composition according to  claim 18  to said subject in need of such treatment. 
     
     
         27 . A method of treating a subject known to suffer from Inflammatory Bowel Disease or Irritable Bowel Syndrome comprising administering a therapeutically effective amount of the controlled release oral pharmaceutical composition according to  claim 19  to said subject in need of such treatment. 
     
     
         28 . A method of treating a subject known to suffer from Inflammatory Bowel Disease or Irritable Bowel Syndrome comprising administering a therapeutically effective amount of the controlled release oral pharmaceutical composition according to  claim 20  to said subject in need of such treatment. 
     
     
         29 . A method of treating a subject known to suffer from Inflammatory Bowel Disease or Irritable Bowel Syndrome comprising administering a therapeutically effective amount of the controlled release oral pharmaceutical composition according to  claim 21  to said subject in need of such treatment. 
     
     
         30 . A method of treating a subject known to suffer from Inflammatory Bowel Disease or Irritable Bowel Syndrome comprising administering a therapeutically effective amount of the controlled release oral pharmaceutical composition according to  claim 22  to said subject in need of such treatment.